3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3β

…, E ter Haar, D Lauffer, J Madden, K Tanner…

Index: Arnost, Michael; Pierce, Al; Haar, Ernst ter; Lauffer, David; Madden, Jaren; Tanner, Kirk; Green, Jeremy Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 5 p. 1661 - 1664

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Citation Number: 40

Abstract

A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3β was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit.